ORIC-101

Research use only, not for human use.

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity.

ORIC-101 (ORIC101) is a highly potent, selective steroidal glucocorticoid receptor (GR) antagonist (IC50=5.6 nM) with reduced androgen receptor (AR) agonistic activity; dose-dependently reduces the expression levels of two established GR target genes, GILZ and FKBP5 with IC50 of 24.9 and 19.5 nM in human PBMCs; demonstrates in vivo antitumor activity by enhancing response to chemotherapy in the GR+ OVCAR5 ovarian cancer xenograft model.Ovarian Cancer Phase 1 Clinical.

ORIC-101 shows markedly reduced androgen receptor agonism (EC50, 2500 nM) and CYP2C8 and CYP2C9 inhibition profiles (IC50, >10 μM).ORIC-101 (1-1000 nM) dose-dependently reduces the expression of n GR-mediated target gene (FKBP5 and GILZ), with IC50s of 17.2 and 21.2 nM, respectively.

ORIC-101 (75 mg/kg, P.O. twice a day for 16-22 days) enhances the anti-tumor activity in combination with gemcitabine and carboplatin in OVCAR5 xenograft tumor in cortisol-treated mice. Animal Model:OVCAR5 xenograft tumor in cortisol-treated mice Dosage:75 mg/kg with 100 mg/kg gemcitabine and 60 mg/kg carboplatin Administration:P.O. twice a day for 16-22 days Result:Significantly reduced tumor volume in combination with chemotherapeutic agents.

ORIC101 | ORIC 101

Endocrinology/Hormones

GR

GR

Cancer

Ovarian Cancer

2222344-98-9

501.755

C34H47NO2

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (199.31 mM)

O=C1CC[C@]2([H])[C@@]3([H])[C@@H](C4=CC=C(N(C(C)C)C)C=C4)C[C@]5(C)[C@](O)(C#CC(C)(C)C)CC[C@@]5([H])[C@]3([H])CCC2=C1

(8R,9S,10R,11S,13S,14S,17S)-17-(3,3-Dimethylbut-1-yn-1-yl)-17-hydroxy-11-(4-(isopropyl(methyl)amino)phenyl)-13-methyl-1,2,6,7,8,9,10,11,12,13,14,15,16,17-tetradecahydro-3H-cyclopenta[a]phenanthren-3-one

(-20℃)

With Ice Pack

≥ 2 years